554-57-4

• 常用中文名：醋甲唑胺
• 常用英文名：Methazolamide
• CAS号：554-57-4
• 分子式：C₅H₈N₄O₃S₂
• 分子量：236.272
• 相关类别： 原料药 泌尿系统用药 利尿药
• 发布时间：2018-04-27 08:00:00
• 更新时间：2024-01-05 13:39:48
• Methazolamide是碳酸酐酶抑制剂，可作用于青光眼。

名称

• 中文名: 醋甲唑胺
• 英文名: Methazolamide
• 中文别名: 醋酸卡泊芬净; N-[(2E)-5-(氨基磺酰基)-3-甲基-1,3,4-噻二唑-2(3H)-亚基]乙酰胺
• 英文别名: N-[(2E)-5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene]acetamide; methazolamide; Methazolamide [BAN:INN:JAN]; Acetamide, N-[(2E)-5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene]-; Methazolamide (JAN/USP); EINECS 209-066-7; N-(4-Methyl-2-sulfamoyl-D2-1,3,4-thiadiazolin-5-ylidene)acetamide; Metazolamide [DCIT]; Acetamide, N-[(2Z)-5-(aminosulfonyl)-3-methyl-1,3,4-thiadiazol-2(3H)-ylidene]-; 5-Acetylamino-4-methyl-D2-1,3,4-thiadiazoline-2-sulfonamide; NEPTAZANE; N1-[5-(aminosulfonyl)-3-methyl-2,3-dihydro-1,3,4-thiadiazol-2-yliden]acetamide; 4-27-00-08221 (Beilstein Handbook Reference); N-[(2Z)-3-Methyl-5-sulfamoyl-1,3,4-thiadiazol-2(3H)-ylidene]acetamide; N-[5-(Aminosulfonyl)-3-methyl-1,3,4-triadiazol-2(3H)-ylidene]acetamide; N-[(2E)-3-Methyl-5-sulfamoyl-1,3,4-thiadiazol-2(3H)-ylidene]acetamide; MFCD00083416; N-(3-methyl-5-sulfamoyl-1,3,4-thiadiazol-2-ylidene)acetamide

物化性质

• 密度: 1.8±0.1 g/cm3
• 沸点: 402.0±28.0 °C at 760 mmHg
• 熔点: 208ºC (dec.)
• 分子式: C₅H₈N₄O₃S₂
• 分子量: 236.272
• 闪点: 196.9±24.0 °C
• 精确质量: 236.003784
• PSA: 144.03000
• LogP: 0.13
• 蒸汽压: 0.0±0.9 mmHg at 25°C
• 折射率: 1.737
• 储存条件: 2-8°C

生物活性

• 描述: Methazolamide是碳酸酐酶抑制剂,可作用于青光眼。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 碳酸酐酶
  研究领域 >> 其他
• 参考文献:

  [1]. Casini, A., et al., Carbonic anhydrase inhibitors: SAR and X-ray crystallographic study for the interaction of sugar sulfamates/sulfamides with isozymes I, II and IV. Bioorg Med Chem Lett, 2003. 13(5): p. 841-5.

  [2]. Kiwull-Schone, H.F., et al., Methazolamide does not impair respiratory work performance in anesthetized rabbits. Am J Physiol Regul Integr Comp Physiol, 2009. 297(3): p. R648-54.

  [3]. Skorobohach, B.J., D.A. Ward, and D.V. Hendrix, Effects of oral administration of methazolamide on intraocular pressure and aqueous humor flow rate in clinically normal dogs. Am J Vet Res, 2003. 64(2): p. 183-7.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : AC6350000 CHEMICAL NAME : Acetamide, N-(4-methyl-2-sulfamoyl-delta(sup 2)-1,3,4-thiadiazolin-5-ylidene)- CAS REGISTRY NUMBER : 554-57-4 BEILSTEIN REFERENCE NO. : 0232387 LAST UPDATED : 199612 DATA ITEMS CITED : 3 MOLECULAR FORMULA : C5-H8-N4-O3-S2 MOLECULAR WEIGHT : 236.29 WISWESSER LINE NOTATION : T5NNYSJ B CUNV1 ESZW HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 2420 mg/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - other changes REFERENCE : JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 18,351,1975 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intravenous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >1 gm/kg TOXIC EFFECTS : Details of toxic effects not reported other than lethal dose value REFERENCE : NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: 6,819,1982 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X7129 No. of Facilities: 10 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 197 (estimated) No. of Female Employees: 59 (estimated)

安全

• 符号: GHS07, GHS08
• 信号词: Warning
• 危害声明: H302 + H312 + H332-H351
• 警示性声明: P261-P280-P301 + P312 + P330
• 危害码 (欧洲): Xn:Harmful
• 风险声明 (欧洲): R20/21/22;R40
• 安全声明 (欧洲): S22-S36
• 危险品运输编码: NONH for all modes of transport
• WGK德国: 3
• RTECS号: AC6350000
• 海关编码: 2935009090

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海关

海关编码	2935009090
中文概述	2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无 最惠国关税:6.5% 普通关税:35.0%
申报要素	品名, 成分含量, 用途
Summary	2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%